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Flashcards covering key vocabulary and concepts from the Cell Signaling lecture notes.
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Signal transduction
A process by which an extracellular signal produces a change in the intracellular state of the target cell and ultimately evokes a response of the target cell
Receptor
Molecule that binds the signal with high affinity
Second messengers
Small molecules that rapidly diffuse the signal inside the cell
Water-soluble second messengers
cAMP, cGMP, Ca2+, IP3
Lipid-soluble second messengers
DAG and PIP3
How intracellular signals are transmitted
Binding to another signaling molecule, Binding to a second messenger, Covalent modifications (phosphorylation, ubiquitylation or other), Binding to GTP/GDP
Types of Signaling Molecules
Small molecules like amino acids and derivatives, Gas, Steroids, derivatives of cholesterol, Eicosanoids, derivatives of arachidonic acid, Polypeptides and proteins
Surface receptors
Coupled to ion channels, Coupled to G proteins, Coupled to enzymes (e.g. tyrosine kinases)
Intracellular receptors
Coupled to transcriptional factors (nuclear receptors), Coupled to enzymes (e.g. guanylyl cyclase)
Surface receptors coupled to ion channels
Ligand-gated channels rapidly convert an extracellular signal into an electrical signal
G protein-coupled receptors (GPCRs)
The largest family of cell surface receptors
GEF
Guanine nucleotide Exchange Factors
GAP
GTPase Activating Protein
αs G protein
Stimulate adenylyl cyclase ↑cAMP
αi/o G protein
Inhibit adenylyl cyclase ↓cAMP
αq/11 G protein
Activate Phospholipase β ↑DAG & Ca2+
α12/13 G protein
Activate Rho-GTPases
βγ G protein
Activate PI3-kinase: ↑PIP3; Also opens K+ channels in heart
cAMP
Effects are mediated by cAMP-dependent protein kinase, or protein kinase A (PKA)
Cellular Adaptation to Signals
Cells can adjust their sensitivity to a signal via receptor sequestration, receptor down-regulation, receptor inactivation, inactivation of signaling protein, and production of inhibitory protein
Agonist
A substance that upon binding to the receptor mimics the action of the ligand
Antagonist
A substance that upon binding to the receptor dampens or blocks the ligand-mediated response.
Phospholipase C (PLC)
Catalyzes the hydrolysis of PIP2 in DAG and IP3
Ca2+ signaling
Increases of cytosolic Ca2+ concentrations evoke many cellular responses through the binding Ca2+-regulated proteins
PIP3
Phosphatidylinositol 3,4,5-trisphosphate evokes signal by targeting proteins containing the pleckstrin homology (PH) domain to the plasma membrane